Abstract
Synthesis, characterization and cytotoxic activities of ten benzothiazole-piperazine derivatives were reported. In vitro cytotoxic activities of compounds were screened against hepatocellular (HUH-7), breast (MCF-7) and colorectal (HCT-116) cancer cell lines by sulphorhodamine B assay. Based on the GI50 values of the compounds, most of the benzothiazole-piperazine derivatives are active against HUH-7, MCF-7 and HCT-116 cancer cell lines. Aroyl substituted compounds 1h and 1j were found to be the most active derivatives. In addition, further investigation of compounds 1h and 1j by Hoechst staining and FACS revealed that these compounds cause apoptosis by cell cycle arrest at subG1 phase.
Keywords: Anticancer, apoptosis, benzothiazole, cytotoxicity, piperazine, sulphorhodamine B.
Anti-Cancer Agents in Medicinal Chemistry
Title:Synthesis and Anticancer Activity Evaluation of Some Benzothiazole-Piperazine Derivatives
Volume: 15 Issue: 3
Author(s): Enise Ece Gurdal, Ebru Buclulgan, Irem Durmaz, Rengul Cetin-Atalay and Mine Yarim
Affiliation:
Keywords: Anticancer, apoptosis, benzothiazole, cytotoxicity, piperazine, sulphorhodamine B.
Abstract: Synthesis, characterization and cytotoxic activities of ten benzothiazole-piperazine derivatives were reported. In vitro cytotoxic activities of compounds were screened against hepatocellular (HUH-7), breast (MCF-7) and colorectal (HCT-116) cancer cell lines by sulphorhodamine B assay. Based on the GI50 values of the compounds, most of the benzothiazole-piperazine derivatives are active against HUH-7, MCF-7 and HCT-116 cancer cell lines. Aroyl substituted compounds 1h and 1j were found to be the most active derivatives. In addition, further investigation of compounds 1h and 1j by Hoechst staining and FACS revealed that these compounds cause apoptosis by cell cycle arrest at subG1 phase.
Export Options
About this article
Cite this article as:
Gurdal Ece Enise, Buclulgan Ebru, Durmaz Irem, Cetin-Atalay Rengul and Yarim Mine, Synthesis and Anticancer Activity Evaluation of Some Benzothiazole-Piperazine Derivatives, Anti-Cancer Agents in Medicinal Chemistry 2015; 15 (3) . https://dx.doi.org/10.2174/1871520615666141216151101
DOI https://dx.doi.org/10.2174/1871520615666141216151101 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
Call for Papers in Thematic Issues
Induction of cell death in cancer cells by modulating telomerase activity using small molecule drugs
Telomeres are distinctive but short stretches present at the corners of chromosomes and aid in stabilizing chromosomal makeup. Resynthesis of telomeres supported by the activity of reverse transcriptase ribonucleoprotein complex telomerase. There is no any telomerase activity in human somatic cells, but the stem cells and germ cells undergone telomerase ...read more
Role of natural compounds as anti anti-cancer agents
Cancer is considered the leading cause of worldwide mortality, accounting for nearly 10 million deaths in 2022. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy remains an important approach in treatment o f several types of cancers, even though ...read more
Signaling and enzymatic modulators in cancer treatment
Cancer accounts for nearly 10 million deaths in 2022 and is considered the leading cause of worldwide mortality. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy, radiotherapy and surgery are the most important approach for the treatment of several ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Newer Avenues for the Treatment of Leptomeningeal Carcinomatosis
Central Nervous System Agents in Medicinal Chemistry Advanced Assessment of the Endogenous Hormone Level as a Potential Biomarker of the Urogenital Tract Cancer
Combinatorial Chemistry & High Throughput Screening Genetic and Epigenetic Regulation of Phosphoinositide 3-kinase Isoforms
Current Pharmaceutical Design Recent Patents on Proteasome Inhibitors of Natural Origin
Recent Patents on Anti-Cancer Drug Discovery Recent Patents on the Identification and Clinical Application of microRNAs and Target Genes
Recent Patents on DNA & Gene Sequences Can Breast Cancer Stem Cells Evade the Immune System?
Current Medicinal Chemistry Alternative Splicing and Tumor Progression
Current Genomics Curcumin: the Yellow Molecule with Pleiotropic Biological Effects
Letters in Drug Design & Discovery Rho-Signaling Pathways in Chronic Myelogenous Leukemia
Cardiovascular & Hematological Disorders-Drug Targets Role of Stem Cells in Normal Liver and Cancer
Anti-Cancer Agents in Medicinal Chemistry Inhibitors of Cyclin Dependent Kinases: Useful Targets for Cancer Treatment
Current Cancer Drug Targets Benzimidazoles: An Ideal Privileged Drug Scaffold for the Design of Multitargeted Anti-inflammatory Ligands
Mini-Reviews in Medicinal Chemistry Animal Modeling of Cancer Pathology and Studying Tumor Response to Therapy
Current Drug Targets Epigenetic Targets and their Inhibitors in Cancer Therapy
Current Topics in Medicinal Chemistry Poly(ADP-ribose)polymerase Inhibition - Where Now?
Current Medicinal Chemistry Chlorophylls and their Derivatives Used in Food Industry and Medicine
Mini-Reviews in Medicinal Chemistry Cytoplasmic CXCR4 High-Expression Exhibits Distinct Poor Clinicopathological Characteristics and Predicts Poor Prognosis in Triple-Negative Breast Cancer
Current Molecular Medicine Epigenetic Modifications Due to Heavy Metals Exposure in Children Living in Polluted Areas
Current Genomics Glycerophospholipid Synthesis as a Novel Drug Target Against Cancer
Current Molecular Pharmacology Novel Therapeutic Strategies for Dementia
CNS & Neurological Disorders - Drug Targets